Ziyuglycoside I isolated from S. officinalis root, has anti-wrinkle activity, and increases the expression of type I collagen. Ziyuglycoside I could be used as an active ingredient for cosmetics[1].Ziyuglycoside I triggers cell cycle arrest and apoptosis mediated by p53, it can be a potential drug candidate for treating triple-negative breast cancer (TNBC)[2].
IRE1α kinase-IN-6 is a potent IRE1α inhibitor with an IC50 value of 4.4 nM.
1,4-Anthraquinone is a potent anticancer agent. 1,4-Anthraquinone blocks nucleoside transport, inhibits macromolecule synthesis, induces DNA fragmentation, and decreases the growth and viability of cancer cells. 1,4-Anthraquinone can be used to research anti-leukemia[1].
Regorafénib N-oxyde-d3(M2) is the deuterium labeled Regorafénib N-oxyde M2[1]. Regorafénib N-oxyde M2 is an active metabolite of Regorafenib. Regorafenib is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively[2].
Cbl-b-IN-6 (Compound 246) is a casitas B-lineage lymphoma-b (Cbl-b) and c-Cbl inhibitor with IC50s of 6.7 nM and 5.2 nM, respectively[1].
PARP7-IN-15 (Compound 18) is a PARP7 inhibitor with IC50 of 0.56 nM, that has antitumor activity[1].
Ethyl orsellinate is a lichen metabolite and a derivative of lecanoric acid with antiproliferative and antitumour activities[1]. Ethyl Orsellinate is against A. salina for the cytotoxic activity with an LC50 of 495 μM[2].
Momordicoside G (Momordicacoside G) is an orally active cucurbitane-type triterpene glycoside. Momordicoside G selectively induces apoptosis of M1-like macrophages, without affecting M2-like macrophages. Momordicoside G reduces intracellular ROS levels and promotes autophagy. Momordicoside G also has anticancer activity, inhibiting the growth of cancer cell lines. Momordicoside G stimulates M2-associated lung injury repair and prevents inflammatory lung cancer injury[1].
Volasertib (BI 6727) trihydrochloride is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib trihydrochloride inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib trihydrochloride induces mitotic arrest and apoptosis. Volasertib trihydrochloride, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models[1][2].
Aceratioside, a tetralin glucoside, is a weakly cytostatic constituent. Aceratioside is an antineoplastic agent[1].
HO-PEG18-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
(±)-Zanubrutinib is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor.
5’-Azido-5’-deoxy-2’-O,4’-C-methyleneuridine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Anticancer agent 75 is a potent anticancer agent. Anticancer agent 75 shows cytotoxicity and selectivity in cancer cell lines. Anticancer agent 75 shows cytotoxicity to normal human kidney cell lines is at least 35 times lower than that of the Doxorubicin standard. Anticancer agent 75 shows good activity of antiplasmodial[1].
Crisnatol (BWA770U) mesylate is an orally active and anticancer agent, and a member of the arylmethylaminopropanediol class of DNA intercalators. Crisnatol mesylate shows in vitro cytotoxicity against human breast cancer cells, but not normal human skin fibroblasts[1][2][3].
Datopotamab (CDP7657) is an antibody targeting to TROP2. Datopotamab can be used to synthesize Datopotamab deruxtecan (HY-141598), TROP2-directed antibody-drug conjugate (ADC). Datopotamab deruxtecan consists of DNA topoisomerase I inhibitor Deruxtecan (HY-13631E) and Datopotamab[1].
MRT-2359 is an orally active and potent degrader of GSPT1 with anti-tumor activity. MRT-2359 also inhibits the growth of resistant non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC) cells. MRT-2359 exhibits preferential activity in MYC-driven cell lines, such as N- and L-MYC high NSCLC and SCLC patient-derived xenografts (PDXs)[1].
NSC 689534 can form copper chelate with Cu2+. NSC 689534/Cu2+ complex is a potent oxidative stress inducer, and has antitumor activity[1].
(3R,5S)-Fluvastatin ((3R,5S)-XU 62-320) sodium is the 3R,5S-isomer Fluvastatin. Fluvastatin (XU 62-320 free acid) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway[1][2][3].
Isothymusin is a potent anti-oxidant agent. Isothymusin shows radical scavenging activities. Isothymusin shows anti-proliferative activities in cancer cell lines. Isothymusin inhibited the enzymes associated with the promotion stage of cancer, including cycloxygenase- 2 and lipoxygenase-5[1][2].
Ailanthone (Δ13-Dehydrochaparrinone) is a potent inhibitor of both full-length androgen receptor (AR) (IC50=69 nM) and constitutively active truncated AR splice variants (AR1-651 IC50=309 nM).
PHA-767491 is a dual Cdc7/Cdk9 inhibitor, with IC50s of 10 nM and 34 nM, respectively.
FLT3/ITD-IN-2 (Compound 17) is a potent FLT3 internal tandem duplications (FLT3-ITD) inhibitor with IC50 values of 0.3, 0.4 and 1.0 nM against FLT3D835Y, FLT3 and FLT3-ITD, respectively. FLT3/ITD-IN-2 potently inhibits the phosphorylation of FLT3 and displays excellent antiproliferative activities against acute myeloid leukemia cell lines[1].
XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, 100 fold selectivity over JAK1; shows good biochemical and cellular potency against JAK2 with good selectivity against the Janus Kinase family as well as a broad kinase panel.IC50 Value: 2.2 nM (JAK2); 214.2 nM (JAK3) [1]XL019 was selected as a clinical candidate and advanced into human clinical trials where it was evaluated in patients with primary myelofibrosis, post-polycythemia vera, or post-essential thrombocythemia myelofibrosis.in vitro: Analogue XL019 was also evaluated against a selectivity panel of 118 kinases. Targets for which XL019 exhibited IC50 <1000 nM are displayed. Overall XL019 is a highly selective JAK2 inhibitor displaying >50-fold selectivity against all kinases tested including JAK family members JAK1 and TYK2. Further in vitro evaluation of XL019 revealed that it demonstrated a desirable CYP (1A2, 2C9, 2D6, 3A4 20 μM), hERG (16 μM), and P-glycoprotein inhibition (>20 μM) profile [1].in vivo: XL019 was administered orally to mice bearing HEL92.1.7 tumors and inhibition of STAT phosphorylation was measured after 4 h. A significant inhibition of downstream markers pSTAT1 and pSTAT3 is observed at 30, 100, and 300 mg/kg resulting in an ED50 of 42 mg/kg (pSTAT1) and 210 mg/kg (pSTAT3). XL019 had a superior pharmacodynamic profile and thus was evaluated in an efficacy experiment measuring growth inhibition of HEL.92.1.7 xenograft tumors in mice. Derivative XL019 demonstrated 60% and 70% inhibition when dosed orally at 200 mg/kg and 300 mg/kg respectively twice a day for 14 days. Harvested tumors were also subjected to immunohistochemical analysis of microvessel density (CD31), proliferation (Ki67) and apoptosis (TUNEL). Dosing at 300 mg/kg bid provided an 11.3-fold increase in apoptosis relative to vehicle control [1].
β-Lactose is the anomeric form of Lactose. β-Lactose is a natural inhibitor of the Galectin-3 protein with potential anti-tumor activity.
Isolugrandoside is a nature product. Isolugrandoside can be isolated from Digitalis davisiana Heywood[1].
KSPWFTTL is an immunodominant Kb-restricted epitope from the p15E transmembrane protein. KSPWFTTL can restore susceptibility of a tumor line to anti-AKR/Gross MuLV cytotoxic T lymphocytes[1][2].
APY29 is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation with IC50 of 280 nM and activates IRE1α RNase activity.
Ensituximab (NEO-102; NPC-1C) is a chimeric monoclonal IgG1 antibody targeting a variant of MUC5AC. Ensituximab shows specificity to colorectal and pancreatic cancer[1][2].
Psoralen(Furocoumarin) is an active ingredient from Fructus Psoraleae; has anticancer activity.IC50 value:Target:in vitro: Psoralen dosages of 1-10 μM exhibited low cytotoxicity toward chondrocytes. However, a dosage of 100 μM suppressed the proliferation of chondrocytes. Different concentrations of psoralen treatments on chondrocytes revealed that GAG and Type II collagen synthesis increased, especially at 100 μM, by 0.39-fold and 0.48-fold, respectively, on day 3, and by 0.51-fold and 0.56-fold, respectively, on day 9 [1]. in vivo: Tumor volume inhibition rates were 43.75% and 40.18%, respectively, in the psoralen and isopsoralen low-dose groups, and tumor weight inhibition rates were 38.83% and 37.77%. Tumor volume inhibition rates were 67.86% and 66.96%, respectively, in the psoralen and isopsoralen high-dose groups, and tumor weight inhibition rates were 49.47% and 47.87% [2]. psoralen can inhibit metastasis of breast cancer to bone in vivo. Histological, molecular biological, and imaging analyses revealed that psoralen inhibits bone metastases in mice [3].